Tetrahydrobenzothiophene carboxamides: Beyond the kinase domain and into the fatty acid realm

[Display omitted] A series of tetrahydrobenzothiophene carboxamides, inspired by structural features present in kinase and SCD1 inhibitors, are presented here. Prototype compound 8 (MMDD13) modulates fatty acid elongase and desaturase indexes, lipid accumulation, while preserving kinase inhibitory a...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-09, Vol.27 (18), p.4462-4466
Hauptverfasser:	Llona-Minguez, Sabin, Fayezi, Shabnam, Alihemmati, Alireza, Juárez-Jiménez, Jordi, Piedrafita, F. Javier, Helleday, Thomas
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetyltransferases - metabolism Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fatty Acid Desaturases - metabolism Fatty Acids - metabolism Humans Molecular Structure Protein Kinases - metabolism Stearoyl-CoA Desaturase - antagonists & inhibitors Stearoyl-CoA Desaturase - metabolism Structure-Activity Relationship Thiophenes - chemical synthesis Thiophenes - chemistry Thiophenes - pharmacology
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Zusammenfassung:	[Display omitted] A series of tetrahydrobenzothiophene carboxamides, inspired by structural features present in kinase and SCD1 inhibitors, are presented here. Prototype compound 8 (MMDD13) modulates fatty acid elongase and desaturase indexes, lipid accumulation, while preserving kinase inhibitory activity. This chemotype represents a stepping stone towards chemical probes to study the consequences of lipid metabolism modulation through non-redundant pathways.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.08.006